The present invention relates to corticoid 21-derivatives.
Water-soluble derivatives of corticoids are known and have been utilized for a long time in therapy. Such derivatives include, for example, sodium salts of corticoid 21-hemisulfates, corticoid 21-phosphates, corticoid 21-sulfobenzoates, corticoid 21-hemisuccinates and corticoid 21-aminoacylates.
The sodium salts of corticoid 21-hemisulfates, corticoid 21-phosphates and corticoid 21-sulfobenzoates normally form stable, sterilizable and storable solutions. However, they have the disadvantage that, after i.v. administration, they are split only relatively gradually and in most cases even only incompletely into the free corticoids which are the actual active agents. This disadvantage has an especially grave effect in the treatment of life-endagering shock conditions with such preparations.
The sodium salts of corticoid 21-hemisuccinates and corticoid 21-aminoacylates, on the other hand, are very rapidly cleaved after i.v. administration, so that the actual active corticoids can immediately deploy their full efficacy. The solutions of these compounds, however, are so instable that they cannot be sterilized at high temperature or stored at room temperature. For this reason, the preparations containing them are always dry powders which must be dissolved shortly before application. This is a serious disadvantage since the danger is rather high than the thus-prepared injection solutions will not be sterile, and that a portion of the active ingredient will remain undissolved.